eluxadoline [Ligand Id: 7691] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2159122 (Eluxadoline, JNJ-27018966, Truberzi, Viberzi) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| ChEMBL | Agonist activity at delta opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 4869-4872 [PMID:22695132] |
| δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
| ChEMBL | Binding affinity to rat delta opioid receptor | B | 8.89 | pKi | 1.3 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 4869-4872 [PMID:22695132] |
| GtoPdb | - | - | 8.89 | pKi | 1.3 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 4869-72 [PMID:22695132] |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Binding affinity to guinea pig kappa opioid receptor | B | 7.26 | pKi | 55 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 4869-4872 [PMID:22695132] |
| ChEMBL | Agonist activity at kappa opioid receptor guinea pig colon tissue | F | 5.8 | pEC50 | 1600 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 4869-4872 [PMID:22695132] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| GtoPdb | - | - | 8.77 | pKi | 1.7 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 4869-72 [PMID:22695132] |
| ChEMBL | Agonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay | F | 9 | pEC50 | 1 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 4869-4872 [PMID:22695132] |
| μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | Binding affinity to rat mu opioid receptor | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 4869-4872 [PMID:22695132] |
| GtoPdb | - | - | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 4869-72 [PMID:22695132] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
